Journal ArticleDOI
Histone deacetylase inhibitors.
TLDR
Design of a second generation ofHDACs was based upon data affording potent HDACs such as LAQ824 and PDX101 currently under phase I clinical trials, and two of them, MS-275 and CI-994, have reached phase II and I clinical Trials, respectively.About:
This article is published in European Journal of Medicinal Chemistry.The article was published on 2005-01-01. It has received 819 citations till now. The article focuses on the topics: Histone deacetylase & Phenylbutyrate.read more
Citations
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Hydroxyurea and hydroxamic acid derivatives as antitumor drugs.
Nina Saban,Maro Bujak +1 more
TL;DR: Hydroxyurea has been used for decades but nowadays the main focus has shifted to structurally similar hydroxamic acid derivatives that target specific enzymes involved in cancer progression such as histone deacetylases, matrix metalloproteinases and also RNR.
Journal ArticleDOI
Epigenetic Modifications and Head and Neck Cancer: Implications for Tumor Progression and Resistance to Therapy.
TL;DR: The understanding and characterization of epigenetic modifications associated with head and neck carcinogenesis, and the prospective identification of epigenetics markers associated with CSCs, hold the promise for novel therapeutic strategies to fight tumors.
Journal ArticleDOI
Histone deacetylase inhibitors: biology and mechanism of action.
Janice M. Mehnert,Wm Kevin Kelly +1 more
TL;DR: Multiple HDACs and histone acetyltransferases are currently under investigation in clinical trials, including vorinostat (suberoylanilide hydroxamic acid), which was recently approved by the U.S. Food and Drug Administration for the treatment ofcutaneous manifestations of cutaneous T-cell lymphoma in patients with progressive, persistent, or recurrent disease on or after 2 systemic therapies.
Journal ArticleDOI
Prolonged treatment with pimelic o-aminobenzamide HDAC inhibitors ameliorates the disease phenotype of a Friedreich ataxia mouse model
Chiranjeevi Sandi,Ricardo Mouro Pinto,Sahar Al-Mahdawi,Vahid Ezzatizadeh,Glenn Barnes,Steve Jones,James R. Rusche,Joel M. Gottesfeld,Mark A. Pook +8 more
TL;DR: It is shown that there is no overt toxicity up to 5 months of treatment and there is amelioration of the FRDA-like disease phenotype, and these results support further assessment of HDAC inhibitors for treatment of Friedreich ataxia.
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Histone deacetylase inhibitors facilitate partner preference formation in female prairie voles
TL;DR: Observations indicate that TSA and mating facilitate partner preference through epigenetic events, providing, to the best of the knowledge, the first direct evidence for epigenetic regulation of pair-bonding.
References
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Journal ArticleDOI
Crystal structure of the nucleosome core particle at 2.8 Å resolution
TL;DR: The X-ray crystal structure of the nucleosome core particle of chromatin shows in atomic detail how the histone protein octamer is assembled and how 146 base pairs of DNA are organized into a superhelix around it.
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hSIR2SIRT1 Functions as an NAD-Dependent p53 Deacetylase
Homayoun Vaziri,Scott K. Dessain,Scott K. Dessain,Elinor Ng Eaton,Shin-ichiro Imai,Roy A. Frye,Tej K. Pandita,Leonard Guarente,Robert A. Weinberg +8 more
TL;DR: It is proposed that hSir2, the human homolog of the S. cerevisiae Sir2 protein known to be involved in cell aging and in the response to DNA damage, binds and deacetylates the p53 protein with a specificity for its C-terminal Lys382 residue.
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Negative Control of p53 by Sir2α Promotes Cell Survival under Stress
Jianyuan Luo,Anatoly Y. Nikolaev,Shin-ichiro Imai,Delin Chen,Fei Su,Ariel L. Shiloh,Leonard Guarente,Wei Gu +7 more
TL;DR: It is shown that mammalian Sir2alpha physically interacts with p53 and attenuates p53-mediated functions, and Nicotinamide inhibits an NAD-dependent p53 deacetylation induced by Sir2 alpha, and also enhances the p53 acetylation levels in vivo.
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Potent and specific inhibition of mammalian histone deacetylase both in vivo and in vitro by trichostatin A.
TL;DR: Results clearly indicate that TSA is a potent and specific inhibitor of the histone deacetylase and that the in vivo effect of TSA on cell proliferation and differentiation can be attributed to the inhibition of the enzyme.
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Valproic acid defines a novel class of HDAC inhibitors inducing differentiation of transformed cells
Martin Göttlicher,Saverio Minucci,Ping Zhu,Oliver H. Krämer,Annemarie Schimpf,Sabrina Giavara,Jonathan P. Sleeman,Francesco Lo Coco,Clara Nervi,Pier Giuseppe Pelicci,Thorsten Heinzel +10 more
TL;DR: Valproic acid induces differentiation of carcinoma cells, transformed hematopoietic progenitor cells and leukemic blasts from acute myeloid leukemia patients, and tumor growth and metastasis formation are significantly reduced in animal experiments, suggesting that it might serve as an effective drug for cancer therapy.